Title of article
Challenges in the development of mGluR5 positive allosteric modulators: The discovery of CPPHA
Author/Authors
Zhijian Zhao، نويسنده , , David D. Wisnoski، نويسنده , , Julie A. O’Brien، نويسنده , , Wei Lemaire، نويسنده , , David L. Williams Jr.، نويسنده , , Marlene A. Jacobson، نويسنده , , Marion Wittman، نويسنده , , Sookhee N. Ha، نويسنده , , Herve Schaffhauser، نويسنده , , Cyrille Sur، نويسنده , , Doug J. Pettibone، نويسنده , , Mark E. Duggan، نويسنده , , P. Jeffrey Conn، نويسنده , , George D. Hartman، نويسنده , , Craig W. Lindsley، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2007
Pages
6
From page
1386
To page
1391
Abstract
This Letter describes, for the first time, the synthesis and SAR, developed through an iterative analog library approach, that led to the discovery of the positive allosteric modulator (PAM) of the metabotropic glutamate receptor mGluR5 CPPHA. Binding to a unique allosteric binding site distinct from other mGluR5 PAMs, CPPHA has been the focus of numerous pharmacology studies by several laboratories.
Keywords
Allosteric modulator , Potentiation , mGluR5
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2007
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
797855
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